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CDK2 inhibitor II. Group: Biochemicals. Alternative Names: 4- [2- (5-Bromo-1, 2-dihydro-2-oxo-3H-indol-3-ylidene) hydrazinyl] benzenesulfonamide; 4- [ (5-Bromo-1, 2-dihydro-2-oxo-3H-indol-3-ylidene) hydrazino] benzenesulfonamide; SC 221409. Grades: Highly Purified. CAS No. 222035-13-4. Pack Sizes: 5mg. Molecular Formula: C14H11BrN4O3S, Molecular Weight: 395.23. US Biological Life Sciences.
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CDK2 Inhibitor II
The cyclin-dependent kinase 2 (Cdk2) works with cyclins A or E to regulate S phase and G2-M transition during the cell cycle. Cdk2 Inhibitor II is a potent, cell-permeable, ATP-competitive, and selective inhibitor of Cdk2. It is a 3-(benzylidne)indolin-2-one analog that selectively and potently inhibits Cdk2 with IC50 of 60 nM. Synonyms: Cyclin-dependent kinase 2 Inhibitor II; SC-221409. Grade: ≥95%. CAS No. 222035-13-4. Molecular formula: C14H11BrN4O3S. Mole weight: 395.2.
Cdk2 Inhibitor II - CAS 222035-13-4
The Cdk2 Inhibitor II, also referenced under CAS 222035-13-4, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk2 Inhibitor III - CAS 199986-75-9
The Cdk2 Inhibitor III, also referenced under CAS 199986-75-9, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
1-Naphthyl PP1
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1. CAS No. 221243-82-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941.
1-Naphthyl PP1
Selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl. (IC50 values are 1.0, 0.6, 0.6, 18 and 22 uM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). Preferentially inhibits mutant over wild-type kinases (IC50 values are 1.5 vs 1000 nM for I338G v-src and v-src respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 221243-82-9. Pack Sizes: 10mg, 50mg. Molecular Formula: C19H19N5. US Biological Life Sciences.
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1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1 hydrochloride. CAS No. 956025-47-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941B.
1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases, including v-Src and c-Fyn, tyrosine kinase c-Abl and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively. It was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. It was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Uses: 1-naphthyl pp1 hydrochloride could potently block prostate cancer cell proliferation by inducing g2/m arrest. Synonyms: 1-Tert-butyl-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyriMidin-4-aMine hydrochloride; 1-NA-PP 1 hydrochloride. Grade: >98 %. CAS No. 956025-47-1. Molecular formula: C19H20ClN5. Mole weight: 353.85.
AT7519 trifluoroacetate
AT7519 is an ATP competitive CDK inhibitor with a Ki value of 38 nM for CDK1. AT7519 is inactive against all non-CDK kinases with the exception of GSK3β (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620 consistent with the inhibition of CDK1 and CDK2. AT7519 induces dose-dependent cytotoxicity in multiple myeloma (MM) cell lines with IC50 values ranging from 0.5 to 2 μM at 48 hours, with the most sensitive cell lines being MM.1S (0.5 μM) and U266 (0.5 μM) and the most resistant MM.1R (>2 μM). It does not induce cytotoxicity in peripheral blood mononuclear cells (PBMNC). AT7519 partially overcomes the proliferative advantage conferred by IL6 and IGF-1 as well as the protective effect of bone marrow stromal cells (BMSCs). AT7519 induces rapid dephosphorylation of RNA pol II CTD at serine 2 and serine 5 sites, and leads to the inhibition of transcription, partially contributing to AT7519 induced cytotoxicity of MM cells. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. A twice daily dosing of AT7519 (9.1 mg/kg) causes tumor regression of both early-stage and advanced-stage s.c. tumors in the HCT116 and HT29 colon cancer xenograft models. AT7519 treĀ
AUZ 454
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins. Uses: Scientific research. Group: Signaling pathways. Alternative Names: K03861. CAS No. 853299-07-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15004.
Butyrolactone I
It is one of a family of three butyrolactones isolated from aspergillus fumigatus. It exhibits antitumor activity and inhibits the cell cycle at the G1/S and G2/M transitions. It is a selective inhibitor of cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5. Synonyms: Olomoucin; 4'-O-Demethylversicolactone D; (2R)-2,5-Dihydro-4-hydroxy-2-[[4-hydroxy-3-(3-methyl-2-butenyl)phenyl]methyl]-3-(4-hydroxyphenyl)-5-oxo-2-furancarboxylic Acid Methyl Ester; (+)-3''-Dimethylallyl-butyrolactone II. Grade: >95% by HPLC. CAS No. 87414-49-1. Molecular formula: C24H24O7. Mole weight: 424.44.
CAY10574
Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10574, also known as Cdk9 Inhibitor II, is a potent, selective inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with Ki of 13.3 μM and IC50 values 20 μM. Synonyms: CAY 10574; CAY-10574; Cdk9 Inhibitor II. Grade: ≥95%. CAS No. 140651-18-9. Molecular formula: C9H10N6O. Mole weight: 218.2.
CDK12-IN-2
CDK12-IN-2, a potent and selective nanomolar CDK12 inhibitor (IC50 = 52 nM) with good physicochemical properties, inhibits phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, and can be used as an excellent chemical probe for the study of CDK12 function. It is also a strong CDK13 inhibitor because CDK13 is the closest homologue of CDK12. It shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. Synonyms: Urea, N-[trans-4-[(5-cyano-2-pyridinyl)amino]cyclohexyl]-N-[4-(1,6-dihydro-1-methyl-6-oxo-3-pyridinyl)phenyl]-N'-(phenylmethyl)-; 3-Benzyl-1-(trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl)urea. CAS No. 2244987-03-7. Molecular formula: C32H32N6O2. Mole weight: 532.64.
CVT-313
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC 50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Cdk2 Inhibitor III. CAS No. 199986-75-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-15339.
IIIM-290
IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1, respectively. Synonyms: 2-[(E)-2-(2,6-Dichlorophenyl)vinyl]-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-chromen-4-one; 4H-1-Benzopyran-4-one, 2-[(E)-2-(2,6-dichlorophenyl)ethenyl]-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-. Grade: ≥95%. CAS No. 2213468-64-3. Molecular formula: C23H21Cl2NO5. Mole weight: 462.32.
Staurosporin
Staurosporine is an alkaloid isolated from the culture broth of Streptomyces staurospores and is a super-potent, cell permeable PKC inhibitor (IC50=0.7); at higher concentrations Staurosporine inhibits other protein kinases: CDK2/cyclin A (IC50=7uM) and CDK4/cyclin D (IC50=3-10uM). At a concentration of 50-100nM it is a functional neurotrophins agonist promoting neurite outgrowth in neuroblastoma, pheochromocytoma and brain primary neuronal cultures. Staurosporine inhibits a variety of kinases including PKA, PKG, MLCK, CaMK, tyrosine kinases, and phosphorylase kinase. This compound displays selectivity toward the PKC isoforms, inhibiting PKCα, PKC β, PKCγ, PKCδ, and PKCε, but not PKC?, and induces PKC translocation. Staurosporine also inhibits topoisomerase II directly by interaction with the ATP binding site, augments PMA-induced ornithine decarboxylase, and activates a bcl-2-regulated apoptosis pathway. Source:Streptomyces staurosporeus. Group: Biochemicals. Alternative Names: Antibiotic AM2282; Antibiotic 230; CCRIS 3272. Grades: Highly Purified. CAS No. 62996-74-1. Pack Sizes: 100ug, 1mg, 5mg, 10mg. Molecular Formula: C28H26N4O3, Molecular Weight: 466.53. US Biological Life Sciences.
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YKL-5-124
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1957203-01-8. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-101257.
Bisindolylmaleimide III
Potent and selective protein kinase C (PKC) inhibitor. Inhibits panel of protein kinases (e.g. GSK-3beta, CDK2). Group: Biochemicals. Grades: Highly Purified. CAS No. 137592-43-9. Pack Sizes: 1mg, 5mg. Molecular Formula: C23H20N4O2. US Biological Life Sciences.
Worldwide
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